SB431542

製品コード：S1067 純度：99.99%

SB431542 は強力かつ選択的 ALK5 阻害剤であり、cell-free assay における IC50 は 94 nM です。p38 MAPK などのキナーゼよりも ALK5 に対して 100 倍の選択性を有しています。

CAS No. 301836-41-9

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 37000	国内在庫あり
10mg	JPY 29500	国内在庫あり
50mg	JPY 115500	国内在庫あり
200mg	JPY 220500	国内在庫あり
1g	JPY 445500	国内在庫あり

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（706）

製品安全説明書

現在のバッチを見る：純度： 99.99%

99.99

SB431542と併用されることが多い化合物

LDN-193189

SB431542 and LDN-193189, along with other small molecules, reduce the expression of epithelial-mesenchymal cell transition (EMT) marker genes and effectively inhibit fibrosis of liver cells.

Xiang C, et al. Science. 2019 Apr 26;364(6438):399-402.

Y-27632 2HCl

SB431542 and Y-27632 2HCl combination reverse the mesenchymal actin cytoskeleton stress fibers induced by TGF-β1 in TGF-β1 knockout mice cells (mTEC-KO).

Das S, et al. BMC Cell Biol. 2009 Dec 21;10:94.

DMH1

SB431542 and DMH1 combined use regulates the two TGF-β signaling pathways independently in human-induced pluripotent stem cells (hiPSCs).

Neely MD, et al. ACS Chem Neurosci. 2012 Jun 20;3(6):482-91.

SU5402

SB431542 and SU5402 block NODAL and FGF9 signalling that allows germ cells to differentiate in Emx2-knockdown testes in vitro.

Tian-Zhong M, et al. Reproduction. 2016 Jun;151(6):673-81.

Laduviglusib (CHIR-99021)

SB431542 and Laduviglusib suppress the gene expressions of pluripotent-related transcription factors and epithelial‑mesenchymal transition (EMT)-related genes to various levels in HeLa cells.

Zhang Y, et al. Oncol Rep. 2019;41(6):3545-3554.

SB431542関連製品

関連ターゲット	ALK1 ALK2 ALK3 ALK4 TGFβRI/ALK5 ALK6 TGFβRII TGF-β Smad3 Smad4 Smad5 ALK7	もっと見る
関連製品	LDN-193189 Galunisertib (LY2157299) LY2109761 SB525334 LDN-193189 2HCl SIS3 HCl RepSox (E-616452) LY364947 DMH1 SB505124 GW788388 A-83-01 SD-208 K02288 Vactosertib (TEW-7197) SIS3 Kartogenin ITD-1 LDN-212854 LY 3200882 ML347 TP0427736 HCl SRI-011381 (C381) LDN-214117 Hesperetin Alantolactone TGFβRI-IN-3 Anti-human/mouse TGF-β-InVivo	もっと見る
関連化合物ライブラリー	Kinase Inhibitor Library PI3K/Akt Inhibitor Library MAPK Inhibitor Library Cell Cycle compound library TGF-beta/Smad compound library	もっと見る

シグナル伝達経路

TGF-beta/Smadシグナル伝達経路

TGF-beta/Smad阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
Mouse embryo cardiomyocytes	Function Assay	10 μM	1 h	Inhibits Trypanosoma cruzi Dm28C infection-induced Smad2 phosphorylation in mouse embryo cardiomyocytes at 10 uM	17526757
Mouse embryo cardiomyocytes	Function Assay	10 μM	1 h	Inhibits TGF-beta-1-induced Smad2 phosphorylation in mouse embryo cardiomyocytes at 10 uM	17526757
Mouse embryo cardiomyocytes	Function Assay	10 μM	1 h	Inhibits invasion of Trypanosoma cruzi Y in mouse embryo cardiomyocytes assessed as pathogen infection at 10 uM	17526757
C32	Function Assay	10 μM	20h	Inhibits Trypanosoma cruzi Y infection-induced TGFbeta signaling in mink C32 cells at 10 uM	17526757
CHO-HIR	Function Assay	0.01-3 μM	2 h	Inhibits TGFbeta-induced downstream transcriptional activation of ALK5 expressed in CHO-HIR cells assessed as intracellular translocation of EGFP-Smad2 with IC50 of 0.35μM	24055046
HaCaT	Function Assay	3.2-50 μM	15 min	Inhibits TGFbeta receptor in human HaCaT cells assessed as Smad phosphorylation with IC50 of 0.172μM	20919678
H1299	Migration Assay	1 μM	12-24 h	Induces antimigratory activity against human H1299 cells assessed as Inhibition of cell migration with IC50 of 0.5μM	24417479
HEK293T	Function Assay	10 μM	22 h	Inhibits TGBR2 signaling in human HEK293T cells assessed as Inhibition of SMAD activation with IC50 of 0.066μM	23130626
Trypanosoma cruzi trypomastigotes	Antimicrobial Assay	10 μM	4 h	Induces antitrypanosomal activity against Trypanosoma cruzi trypomastigotes assessed as effect on parasite morphology at 10 uM	17526757
Mouse cardiomyocytes	Antimicrobial Assay	10 μM	4 h	Induces antitrypanosomal activity against Trypanosoma cruzi Y in mouse cardiomyocytes assessed as reduction of intracellular amastigotes at 10 uM	17526757
Mouse cardiomyocytes	Antimicrobial Assay	10 μM	96 h	Induces antitrypanosomal activity against Trypanosoma cruzi Y in mouse cardiomyocytes assessed as Inhibition of trypomastigote release at 10 uM	17526757
HaCaT	Function Assay	0.05 μM	2 h	Does not inhibit TGF-beta induced ALK5 activity in HaCaT cells assessed as p3TP-luciferase reporter activity at 0.05 uM	17552507
Sf9	Function Assay		2 h	Inhibits human recombinant ALK5 phosphorylation expressed in Sf9 cells with IC50 of 1.542μM	17552507
HepG2	Function Assay		12 h	Inhibits TGFR-1 in human HepG2 cells expressing PAI-luciferase with IC50 of 0.25μM	19914068
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生物活性

製品説明

Targets

ALK4 ^[2] (Cell-free assay)	ALK7 ^[2] (Cell-free assay)	ALK5 ^[1] (Cell-free assay)
		94 nM

In Vitro
In vitro	SB 431542 inhibits the activin type I receptor ALK4 and the nodal type I receptor ALK7, which are responsible for the phosphorylation of Smad2. SB 431542 has little effect on ALK1, ALK2, ALK3, and ALK6, which show phosphorylation of Smad1. SB 431542 is a selective inhibitor of endogenous activin but has no apparent effect on BMP signaling. SB 431542 could induce both Smad2/Smad4- and Smad3/Smad4-dependent transcription. ^[2] In A498 cells, SB 431542 inhibits both TGF-β1-induced collagen Iα1 and PAI-1 mRNA with IC50 of 60 nM and 50 nM, respectively. In addition, SB 431542 inhibits production of TGF-β1-induced fibronectin mRNA and protein with IC50 of 62 nM and 22 nM, respectively. ^[3] SB 431542 blocks the TGF-β-mediated growth factors, including PDGF-A, FGF-2 and HB-EGF, leading to an increase in proliferation of MG63 cells. SB 431542 also inhibits TGF-β-induced c-Myc and p21 ^WAF1/CIP1. ^[4] SB 431542 significantly suppresses TGF-β-induced G1 arrest, leading to accumulation of cells in the S phase of the cell cycle in FET, RIE, and Mv1Lu cells. SB 431542 also inhibits TGF-β-induced epithelial to mesenchymal transition (EMT) in NMuMG and PANC-1 cells. ^[5] SB 431542 significantly elevates the expression of CD86 in BM-DCs and that of CD83 within CD11c+ cells suppressed by TGF-β. SB 431542 is able to induce NK activity through functional maturation and IL-12 production of human DCs. ^[6]
Kinase Assay	Flashplate assay for ALK5
Kinase Assay	SB 431542 is dissolved in DMSO at a concentration of 10 mM. The kinase domain of TGFβRI, from amino acid 200 to the C-terminus, and the full-length Smad3 protein are expressed as N-terminal glutathion S-transferase (GST) fusion proteins in the baculovirus expression system. Proteins are purified with glutathion Sepharose beads 4B. Basic FlashPlates are coated with 0.1 M sterile filtered sodium bicarbonate, pH 7.6, containing 700 ng of GST-Smad3 per 100 μL. Assay buffer contains 50 mM HEPES (pH 7.4), 5 mM MgCl₂, 1 mM CaCl₂, 1 mM DTT, 100 mM GTP, 3 μM ATP plus 0.5 μCi/well ɤ³³P-ATP, and 85 ng of GST-ALK5 with or without SB 431542. Plates are incubated at 30 °C for 3 hours. The assay buffer is removed by aspiration, and the plate is counted on a Packard TopCount 96-well scintillation plate reader.
細胞実験	細胞株	MG63 and NIH3T3
	濃度	0.3 μM
	反応時間	30 minutes
	実験の流れ	To explore the effects of ligands, MG63 and NIH3T3 cells are seeded at a density of 8 × 10⁴ cells/well in 6-well plates and starved (0.1% FCS for MG63 cells and 0.5% FCS for NIH3T3 cells) for 24 hours before ligand stimulation. Media containing various ligands are exchanged at 48-hours intervals. Cells are trypsinized and counted by a Coulter counter on days 2, 4, and 6 after ligand stimulation. To explore the effects of constitutively active receptors, cells are seeded at a density of 2 × 10⁵ cells/well in 6-well plates. The next day, cells are infected with adenoviruses carrying various cDNAs at a multiplicity of infection of 100. Cells are trypsinized and counted on day 3. Cell proliferation assay is performed in the presence of 0.3 μM SB 431542.
実験結果図	Methods	Biomarkers	結果図	PMID
	Western blot	phospho-SMAD3 / Phospho-p38 Y397 phospho-FAK pSmad2 / p-AKT / E-cadherin / vimentin / snail / slug CK18 / Fibronectin / Vimentin		17113264
	Growth inhibition assay	Cell viability		28125630
	Immunofluorescence	Smad2/3		19619490
	Immunofluorescence	Na+/K+-ATPase		23451286
	ELISA	collagen 1		23451286

In Vivo
In Vivo	SB 431542 triggers cytotoxic T lymphocyte (CTL) activities in the colon-26 carcinoma models and is most likely to produce antitumor immunological outcomes through alteration of DC function suppressed by TGF-β. ^[6]
動物実験	動物モデル	BALB/c mice receive intraperitoneal (i.p.) injections of colon-26 tumor cells.
	投与量	1 μM solution, 100 μL/mouse
	投与経路	Directly injected into peritoneal cavity

参考
[1] Callahan JF, et al. J Med Chem, 2002, 45(5), 999-1001. [2] Inman GJ, et al. Mol Pharmacol, 2002, 62(1), 65-74. [3] Laping NJ, et al. Mol Pharmacol, 2002, 62(1), 58-64. [4] Matsuyama S, et al. Cancer Res, 2003, 63(22), 7791-7798. [5] Halder SK, et al. Neoplasia, 2005, 7(5), 509-521. [6] Tanaka H, et al. Oncol Rep, 2010, 24(6), 1637-1643. + 展開

参考

+ 展開

化学情報

分子量	384.39	化学式	C₂₂H₁₆N₄O₃
CAS No.	301836-41-9	SDF	Download SB431542 SDFをダウンロードする
Smiles	C1OC2=C(O1)C=C(C=C2)C3=C(NC(=N3)C4=CC=C(C=C4)C(=O)N)C5=CC=CC=N5
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	１ケ月-20°Cin solvent

In vitro
Batch:

DMSO : 77 mg/mL ( (200.31 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : 3 mg/mL

Water : Insoluble

モル濃度計算器

in vivo Batch: Add solvents to the product individually and in order.					投与溶液組成計算機
	Clear solution	0.1%DMSO 1 99.80% Saline	0.02mg/ml (0.05mM)	Taking the 1 mL working solution as an example, add 1 μL of 20 mg/ml clear DMSO stock solution to 998 μL of Saline and mix evenly. The mixed solution should be used immediately for optimal results.	投与溶液組成計算機
Clear solution	5%DMSO 1 40%PEG 300 2 5%Tween80 3 50% ddH2O	4.0mg/ml (10.41mM)	Taking the 1 mL working solution as an example, add 50 μL of 80 mg/mL clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween-80 to the above system, mix evenly to clarify it; then Continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 95% Corn oil	4.0mg/ml (10.41mM)	Taking the 1 mL working solution as an example, add 50 μL of 80 mg/mL clarified DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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よくある質問（FAQ）

質問1:
I would appreciate it if you can help me in figuring out the formulation for this drug in vivo experiments.

回答
S1067 SB431542 in 1% DMSO+30% polyethylene glycol+1% Tween 80 at 30 mg/ml is a suspension for oral gavage. It can also be dissolved in 2% DMSO+30% PEG 300+ddH2O at 5 mg/ml as a clear solution for IP injection.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):